Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
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Patent number: 9725442Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 24, 2012Date of Patent: August 8, 2017Assignee: SHIONOGI & CO., LTD.Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
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Patent number: 9700551Abstract: The present invention relates to the new use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta (GSK-3?) inhibitors and to their use in the treatment of GSK-3?-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.Type: GrantFiled: August 13, 2015Date of Patent: July 11, 2017Assignee: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Barbara Garofalo, Guido Furlotti, Gabriele Magaro', Rosella Ombrato, Francesca Mancini
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Patent number: 9694014Abstract: Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.Type: GrantFiled: July 15, 2013Date of Patent: July 4, 2017Assignee: Universita Degli Studi di PadovaInventors: Paolo Bonaldo, Marcella Canton, Fabio DiLisa, Sara Menazza
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Patent number: 9676783Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: GrantFiled: September 4, 2015Date of Patent: June 13, 2017Assignee: Array BioPharma, Inc.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 9676768Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: March 20, 2015Date of Patent: June 13, 2017Assignee: ASTEX THERAPEUTICS LIMITEDInventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
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Patent number: 9676771Abstract: A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is N, C(OH), or CH; Y is H or OH; each of Z1-Z5 is independently H or halogen; R4 is H, OH, NH2, NHR8, NR8R9 or R8; R5, R6, and R7 is each independently H, halogen, OR8, R8, NHR8, NR8R9, CO2R8, CONR8R9, SO2NR8R9, or R5 and R6 together with the carbon atoms to which R5 and R6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and R8 and R9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R8 and R9 together with the nitrogen tType: GrantFiled: May 13, 2014Date of Patent: June 13, 2017Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Xue Zhi Zhao, Steven Smith, Mathieu Metifiot, Barry Johnson, Christophe Marchand, Stephen H. Hughes, Yves Pommier, Terrence R. Burke, Jr.
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Patent number: 9657023Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.Type: GrantFiled: July 29, 2014Date of Patent: May 23, 2017Assignee: Gilead Connecticut, Inc.Inventors: Tim G. Elford, Peter Chee-Chu Fung, Michael Laird Hurrey, Dimitrios Stefanidis, Dragos Vizitiu
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Patent number: 9624201Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.Type: GrantFiled: December 10, 2014Date of Patent: April 18, 2017Assignees: HOFFMANN-LA ROCHE INC., CHUGAI PHARMACEUTICAL CO.Inventors: Francisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
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Patent number: 9611253Abstract: Solid forms comprising pyrazolylaminoquinazoline, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.Type: GrantFiled: February 27, 2013Date of Patent: April 4, 2017Assignee: Ambit Biosciences CorporationInventor: Timothy David Gross
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Patent number: 9603820Abstract: Therapeutic methods relating to the use of GABA-AT inhibitor compounds for the treatment of hepatocellular carcinoma.Type: GrantFiled: November 9, 2015Date of Patent: March 28, 2017Assignee: Northwestern UniversityInventors: Richard B. Silverman, Yaron Ilan
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Patent number: 9579319Abstract: This invention relates to novel compounds of formula (I). The compounds of the invention are hedgehog pathway antagonists. Specifically, the compounds of the invention are useful as Smoothened (SMO) inhibitors. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of the Hedgehog pathway and SMO, for example cancer.Type: GrantFiled: May 28, 2014Date of Patent: February 28, 2017Assignee: Redx Pharma PLCInventors: Richard Armer, Matilda Bingham, Inder Bhamra, Andrew McCarroll
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Patent number: 9573946Abstract: Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof.Type: GrantFiled: February 19, 2015Date of Patent: February 21, 2017Assignees: Novita Pharmaceuticals, Inc., Cornell UniversityInventors: Xin-Yun Huang, Christy Young Shue
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Patent number: 9562013Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.Type: GrantFiled: June 29, 2015Date of Patent: February 7, 2017Assignee: Acetylon Pharmaceuticals, Inc.Inventors: John H. van Duzer, Ralph Mazitschek
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Patent number: 9556150Abstract: This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.Type: GrantFiled: December 10, 2014Date of Patent: January 31, 2017Assignees: Hoffmann-La Roche Inc., Chugai Pharmaceutical Co.Inventors: Francisco Javier Lopez-Tapia, Norman Kong, Sung-Sau So, Yan Lou, Romyr Dominique
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Patent number: 9550770Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions containing the same, and methods of use thereof are described. Specifically quinazoline derivatives of Formula Ia: and their uses in modulating kinase activities are disclosed.Type: GrantFiled: August 22, 2014Date of Patent: January 24, 2017Assignee: NeuPharma, Inc.Inventors: Xiangping Qian, Yong-Liang Zhu
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Patent number: 9539251Abstract: The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.Type: GrantFiled: September 6, 2013Date of Patent: January 10, 2017Assignees: Genentech, Inc., F. Hoffmann-La Roche AGInventors: Deepak Sampath, Christian Klein, Wayne John Fairbrother
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Patent number: 9527818Abstract: Provided are a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a therapeutic agent for gonadotropin-dependent diseases (for example, prostate cancer, breast cancer, endometriosis, uterine fibroid, prostatic hyperplasia, or the like) or a salt thereof, and a synthesis intermediate useful in the production method. The production method of the present invention controls formation of a by-product which is hardly removed unless column purification is conducted and racemization of a target compound, thereby obtaining the target compound with a high purity, and therefore, the production method is suitable for industrial production.Type: GrantFiled: September 6, 2013Date of Patent: December 27, 2016Assignee: Astellas Pharma Inc.Inventors: Takashi Kikuchi, Shinya Yoshida, Atsushi Nakamura, Takahiro Akiba, Toshitaka Yoshino, Shuichi Nakagawa, Kiichi Sato
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Patent number: 9493454Abstract: Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.Type: GrantFiled: September 25, 2013Date of Patent: November 15, 2016Assignees: Tolero Pharmaceuticals, Inc., Mannkind CorporationInventors: Qingping Zeng, Mary Faris, Alexis Mollard, Steven L. Warner, Gary A. Flynn
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Patent number: 9493474Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: GrantFiled: October 25, 2012Date of Patent: November 15, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
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Patent number: 9487506Abstract: Compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the Formula (I), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the Formula (I) are disclosed.Type: GrantFiled: April 11, 2012Date of Patent: November 8, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Ping Lan, Kun Liu, Anthony Ogawa, Hong Shen, Christine Yang, Yuguang Wang, Richard Beresis, Changhe Qi
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Patent number: 9481655Abstract: Methods of inhibiting a receptor tyrosine kinase in a subject in need thereof. Methods of inhibiting the growth of a tumor cell in a subject in need thereof. Methods of treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods of treating HER2 positive breast cancer in a subject in need of treatment for HER2 positive breast cancer. Methods of treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 26, 2014Date of Patent: November 1, 2016Assignee: NATCO PHARMA LIMITEDInventors: Bhujanga rao Adibhatla Kali Satya, Ramanadham Jyothi Prasad, Bollepalli Nageshwara Rao, Nannapaneni Venkaiah Chowdary
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Patent number: 9481675Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: GrantFiled: September 10, 2010Date of Patent: November 1, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Patent number: 9469625Abstract: The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer.Type: GrantFiled: June 22, 2012Date of Patent: October 18, 2016Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Youyi Peng, John Tomesch, Lawrence P. Wennogle, Qiang Zhang
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Patent number: 9458105Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: GrantFiled: November 13, 2013Date of Patent: October 4, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Romyr Dominique, Francisco Javier Lopez-Tapia, Eric Mertz, Sung-Sau So
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Patent number: 9452160Abstract: It is an object of the present invention that the novel nicotinic receptor antagonists disclosed herein may be used in a broad array of clinical or medicinal facets. For example, it is a contemplated use of the present invention that the novel nicotinic receptor antagonists be used to inhibit the growth cycle of non-small cell lung cancer cells. Without being bound by theory, it is an object of the present invention that the nicotinic receptor antagonists disclosed herein are believed to possess reversible binding properties. Moreover, the compounds of the present invention are selective for 0.7 nAChR. For example, the compounds of the present invention are not believed to bind to 0.4 (32 nAChR neuromuscular receptors. It is also contemplated that the nicotinic receptor antagonists of the present invention will be used as a counter measure to treat exposure, or potential exposure, to a wide array of potential neurotoxins.Type: GrantFiled: June 17, 2015Date of Patent: September 27, 2016Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Youyi Peng, Lawrence P. Wennogle, Qiang Zhang, John Tomesch
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Patent number: 9409873Abstract: The invention relates to the compounds and methods for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds and methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.Type: GrantFiled: June 21, 2013Date of Patent: August 9, 2016Assignee: SENEX BIOTECHNOLOGY INC.Inventors: Donald C Porter, Igor B Roninson, Mark P Wentland
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Patent number: 9408842Abstract: The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.Type: GrantFiled: August 20, 2015Date of Patent: August 9, 2016Assignee: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: José-Luis Diaz-Fernández, Ute Christmann
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Patent number: 9388181Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: October 7, 2014Date of Patent: July 12, 2016Assignee: Allergan, Inc.Inventors: Clarence Eugene Hull, III, Thomas C. Malone
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Patent number: 9381171Abstract: A composition including dapsone for preventing or treating a side effect of a steroid in a subject, and methods for preventing or treating a side effect of a steroid using the composition.Type: GrantFiled: December 19, 2014Date of Patent: July 5, 2016Assignee: SAMSUNG ELECTRONICS CO., LTD.Inventors: Sungchun Cho, Sangchul Park
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Patent number: 9370506Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: GrantFiled: May 23, 2014Date of Patent: June 21, 2016Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 9365566Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.Type: GrantFiled: March 25, 2013Date of Patent: June 14, 2016Assignee: Takeda Pharmaceutical Company LimitedInventors: John David Lawson, Mark Sabat, Christopher Smith, Haixia Wang, Young K. Chen, Toufike Kanouni
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Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Patent number: 9353124Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 2, 2013Date of Patent: May 31, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Patent number: 9353126Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: November 13, 2014Date of Patent: May 31, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
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Patent number: 9340532Abstract: Embodiments include compositions and methods of inhibiting CNKSR1 and methods of identifying inhibitors of CNKSR1.Type: GrantFiled: December 16, 2013Date of Patent: May 17, 2016Assignee: Phusis Therapeutics, Inc.Inventors: D. Lynn Kirkpatrick, Martin Indarte, Nathan T. Ihle
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Patent number: 9326987Abstract: The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.Type: GrantFiled: September 6, 2011Date of Patent: May 3, 2016Assignee: Glaxo Group LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Patent number: 9314444Abstract: The present invention relates to a method of treating NASH or NAFLD by delivery of an effective amount of a composition comprising L-glutamine or butyric acid formulated for release in the colon by bypassing the upper digestive tract and stomach.Type: GrantFiled: February 10, 2015Date of Patent: April 19, 2016Assignee: BioKier, Inc.Inventor: Jerzy Ryszard Szewczyk
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Patent number: 9303045Abstract: The present invention provides compounds of the formula: that are 5HT3 receptor antagonists and are therefore useful for the treatment of diseases treatable by inhibition of 5HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: July 16, 2013Date of Patent: April 5, 2016Assignee: Takeda Pharmaceutical Company LimitedInventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
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Patent number: 9290575Abstract: Disclosed herein are method of treating pain using comprising RANK/RANKL antagonists.Type: GrantFiled: November 11, 2014Date of Patent: March 22, 2016Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 9284303Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: GrantFiled: August 6, 2013Date of Patent: March 15, 2016Assignee: Janssen Pharmaceutica N.V.Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
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Patent number: 9278135Abstract: The present invention relates to compounds and methods for treating retroviral infections and/or Hepatitis B viral infections. Some compounds of the invention are described by Formula I: or a stereoisomer, a diastereomer, an enantiomer or racemate thereof.Type: GrantFiled: April 26, 2011Date of Patent: March 8, 2016Assignee: Chimerix Inc.Inventor: Ernest Randall Lanier
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Patent number: 9278081Abstract: The present invention relates to the discovery that compounds isolated from the leaves of the plant Eucalyptus camaldulensis can be used to treat or prevent hyperglycemia and/or hypertension.Type: GrantFiled: October 4, 2013Date of Patent: March 8, 2016Assignee: University of The West IndiesInventors: Denise Daley-Beckford, Trevor Herbert Yee, Ruby Lisa Alexander-Lindo, Paul Bancroft Reese
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Patent number: 9273034Abstract: The meglumine salt of 1-(5,6-dichloro-1H-benzo[d]imidazol-2-yl)-1H-pyrazole-4-carboxylic acid (compound (1)) and pharmaceutically acceptable formulations thereof are described. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity.Type: GrantFiled: October 25, 2012Date of Patent: March 1, 2016Assignee: Janssen Pharmaceutica NVInventors: Kia Sepassi, Michele C. Rizzolio
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Patent number: 9266887Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.Type: GrantFiled: February 6, 2015Date of Patent: February 23, 2016Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
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Patent number: 9255073Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.Type: GrantFiled: May 21, 2013Date of Patent: February 9, 2016Assignee: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
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Patent number: 9241996Abstract: The present invention relates to a method for enhancing the activity of kinase inhibitors in target cells, and more specifically for enhancing the activity of tyrosine kinase inhibitors (TKIs), said method comprising contacting a cell with a kinase inhibitor and a photosensitizing agent and irradiating said cell with light of a wavelength effective to activate the photosensitizing agent, and to the use of this method for enhancing the effects of kinase inhibitors or kinase inhibitor-based drugs in particular to achieve cell death, for example, in cancer treatment and other diseases or conditions in which kinase inhibitors, such as TKIs, have a beneficial effect.Type: GrantFiled: June 26, 2009Date of Patent: January 26, 2016Assignee: PCI BIOTECH ASInventors: Anders Høgset, Anette Weyergang, P{dot over (a)}l Kristian Selbo, Kristian Berg
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Patent number: 9241936Abstract: Disclosed is the use of rupatadine in the manufacture of pharmaceutical composition for preventing or treating chronic obstructive bronchitis, obstructive emphysema or chronic obstructive pulmonary disease. The new medicament, i.e. rupatadine, for treating chronic obstructive pulmonary disease is obvious in therapeutic effects, and low in toxic and side effects, and safe in use in the aspects of treating chronic obstructive bronchitis, obstructive emphysema or chronic obstructive pulmonary disease.Type: GrantFiled: May 18, 2012Date of Patent: January 26, 2016Assignee: BEIJING WEIFENG YIMIN BIO-TECHNOLOGY LIMITED COMPANYInventor: Zhuowei Hu
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Patent number: 9238015Abstract: The present invention relates generally to compositions with a health benefit. In particular, the invention relates to the field of cardiovascular disorders, for example, atherosclerosis, high blood pressure, coronary heart disease, myocardial infarction, angina pectoris, stroke, and heart failure. A subject matter of the invention is a composition comprising 4-oxo-2-pentenoic acid for use in the treatment or prevention of cardiovascular disorders.Type: GrantFiled: March 25, 2013Date of Patent: January 19, 2016Assignee: Nestec S.A.Inventors: Francia Jacqueline Arce Vera, Bertrand Bourqui, Timo Buetler, Stephane Duboux, Francis Foata, Philippe Alexandre Guy, Nicolas Page, Serge Andre Dominique Rezzi
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Patent number: 9175017Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: August 1, 2014Date of Patent: November 3, 2015Inventors: Eric L. Elliott, Abu J. Ferdous, Michael J. Kaufman, Sonja A. Komar, Debra L. Mazaik, Quentin J. McCubbin, Phuong M. Nguyen, Vaithianathan Palaniappan, Raymond D. Skwierczynski, Nobel T. Truong, Csanad M. Varga, Peter N. Zawaneh
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Patent number: 9163032Abstract: The present disclosure relates to esters of 8-[2-(2-pentyl-cyclopropylmethyl)cyclopropyl]-octanoic acid (“DCPLA”). The disclosure further relates to compositions, kits, and methods for treatment using the esters.Type: GrantFiled: November 13, 2012Date of Patent: October 20, 2015Assignee: Blanchette Rockefeller Neurosciences InsituteInventors: Daniel L. Alkon, Thomas J. Nelson
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Patent number: 9161940Abstract: The present invention relates to the long-term administration of a selective estrogen receptor modulator (SERM) with a short half-life for the treatment of a variety of estrogen receptor-mediated conditions. The SERM may be administered at a concentration at or below that of a SERM with a long half-life in order to achieve an equivalent therapeutic effect.Type: GrantFiled: February 14, 2013Date of Patent: October 20, 2015Assignee: REPROS THERAPEUTICS INC.Inventors: Joseph S. Podolski, Ronald D. Wiehle